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| Targets |
CP 43 targets the thousand-and-one amino acid kinases, specifically TAOK1 and TAOK2. It acts as an ATP-competitive inhibitor, binding to the ATP-binding site of these kinases and preventing their activity. By inhibiting TAOK1 and TAOK2, it reduces the phosphorylation of tau at residues S262/S356 and S202/T205/S208, which are implicated in Alzheimer's disease pathology.
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| ln Vitro |
Centrosome-amplified breast cancer cells undergo mitotic cell death and mitosis delay when exposed to TAO kinase inhibitor 1 [1].
In vitro, CP 43 is a potent inhibitor of TAOK1 and TAOK2 with IC50 values of 11 nM and 15 nM, respectively. It inhibits the proliferation of SK-BR-3, BT-549, and MCF-7 breast cancer cells by 94%, 82%, and 46%, respectively, at a concentration of 10 µM. It reduces tau phosphorylation at various residues in kinase assays and in HEK293 cells. The compound inhibits TAOK phosphorylation and activation of JNK in vitro. |
| ln Vivo |
CP 43 has been shown to reduce tau phosphorylation in cortical neurons in a transgenic mouse model of tauopathy and in induced pluripotent stem cell-derived neurons from patients with frontotemporal lobar degeneration. This suggests that inhibition of TAOK1 and TAOK2 may be a therapeutic strategy for tauopathies. It also delays mitosis and increases mitotic cell death in SKBR3 breast cancer cells.
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| Enzyme Assay |
CP 43 is evaluated in cell-free kinase assays using purified TAOK1 and TAOK2 enzymes. The compound is incubated with the kinase, ATP, and a substrate, and the inhibition of kinase activity is measured. IC50 values are determined to quantify the potency of TAOK inhibition. Selectivity is assessed by screening against a broad panel of kinases to determine its off-target effects.
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| Cell Assay |
CP 43 is assessed in cell-based assays using various cancer cell lines, such as SK-BR-3, BT-549, and MCF-7. Cells are treated with CP 43, and cell proliferation is measured to assess its antiproliferative effects. Its effects on tau phosphorylation are evaluated in HEK293 cells by treating them with the compound and measuring phosphorylation at specific residues using Western blot analysis.
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| Animal Protocol |
CP 43 is administered in animal models to evaluate its effects on tau phosphorylation and tauopathy. It has been studied in a transgenic mouse model of tauopathy and in patient-derived iPSC neurons. Efficacy is assessed by measuring tau phosphorylation levels and neurodegeneration markers. The compound is typically formulated for in vivo administration using DMSO or other suitable vehicles.
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| ADME/Pharmacokinetics |
CP 43 has a molecular formula of C25H24N2O2 and a molecular weight of 384.48. Its CAS number is 850467-66-2. The compound is soluble in DMSO. It should be stored under recommended conditions. It is also known as TAO Kinase inhibitor 1 and Compound 43.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for CP 43. The compound is for research use only and is not intended for human therapeutic use. It is a potent and selective TAOK inhibitor used in research to study the role of these kinases in cancer and neurodegenerative diseases.
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| References | |
| Additional Infomation |
CP 43 is a potent and selective inhibitor of TAOK1 and TAOK2. It is also known as TAO Kinase inhibitor 1. It is used in research to study the role of TAOK kinases in cancer and tauopathies such as Alzheimer's disease. It is not approved for clinical use.
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| Molecular Formula |
C25H24N2O2
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|---|---|
| Molecular Weight |
384.479
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| Exact Mass |
384.183
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| CAS # |
850467-66-2
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| PubChem CID |
46673962
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
673.2±54.0 °C at 760 mmHg
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| Flash Point |
224.7±31.4 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.647
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| LogP |
5.37
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
549
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CC(C2=CC=CC=C2C1)NC(=O)CNC(=O)C3=CC=C(C=C3)C4=CC=CC=C4
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| InChi Key |
WQKXOAJVNFOHNZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H24N2O2/c28-24(27-23-12-6-10-20-9-4-5-11-22(20)23)17-26-25(29)21-15-13-19(14-16-21)18-7-2-1-3-8-18/h1-5,7-9,11,13-16,23H,6,10,12,17H2,(H,26,29)(H,27,28)
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| Chemical Name |
N-[2-oxo-2-(1,2,3,4-tetrahydronaphthalen-1-ylamino)ethyl]-4-phenylbenzamide
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| Synonyms |
CP-43; CP43; CP 43
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~162.56 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.41 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6009 mL | 13.0046 mL | 26.0092 mL | |
| 5 mM | 0.5202 mL | 2.6009 mL | 5.2018 mL | |
| 10 mM | 0.2601 mL | 1.3005 mL | 2.6009 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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